Besobrial

Besobrial Uses, Dosage, Side Effects, Food Interaction and all others data.

Alcohol use disorder is responsible for a large worldwide burden of morbidity, premature mortality, and economic consequences resulting from accidents, violence, incarceration, decreased productivity, and increased healthcare spending.

Besobrial, also known by the brand name Campral, is a drug used for the maintenance of alcohol abstinence. It is a structural analogue of the neurotransmitter γ-aminobutyric acid (GABA). Besobrial is the first medication specifically formulated for the maintenance of alcohol abstinence in ethanol-dependent patients after alcohol detoxification, unlike naltrexone and disulfiram. It was first approved by the FDA in 2004 and initially marketed by Forest Laboratories.

Besobrial acts on the CNS, aiding in the restoration of normal glutaminergic neuron activity. Pharmacodynamic studies have shown that acamprosate calcium reduces alcohol intake in alcohol-dependent individuals, likely through effects on NMDA receptors and calcium channels. It is a safe and well-tolerated drug for patients with alcohol dependency and improves the likelihood of alcohol abstinence.

Trade Name Besobrial
Availability Prescription only
Generic Acamprosate
Acamprosate Other Names Acamprosate, Acamprosato, Acamprosatum, N-acetyl homotaurine, N-Acetylhomotaurine
Related Drugs Vivitrol, naltrexone, disulfiram, Antabuse, Campral, Revia
Type
Formula C5H11NO4S
Weight Average: 181.21
Monoisotopic: 181.040878535
Protein binding

Acamprosate is not protein bound. Prescribing information mentions that acamprosate protein binding is negligible.

Groups Approved, Investigational
Therapeutic Class
Manufacturer
Available Country South Africa
Last Updated: September 19, 2023 at 7:00 am
Besobrial
Besobrial

Uses

Besobrial is a medication used to maintain alcohol abstinence in patients with alcohol dependence.

Besobrial is indicated for the maintenance of abstinence from alcohol in patients with alcohol dependence who are abstinent at treatment initiation. It is also indicated for the maintenance of alcohol abstinence in patients who have undergone alcohol detoxification. This drug should be used with a psychosocial support program providing adequate support.

Besobrial is also used to associated treatment for these conditions: Alcohol Abstinence, Alcohol Dependency

How Besobrial works

The mechanism of action of acamprosate for the maintenance of alcohol abstinence has not been established. Chronic alcohol exposure is believed to modify the balance between neuronal excitation and inhibition. Results of studies in animals suggest acamprosate may interact with glutamate and GABA neurotransmitter systems in the CNS, supporting the hypothesis that acamprosate restores the balance between neuronal excitation and inhibition. Evidence shows that acamprosate directly binds and inhibits GABA B receptors and indirectly affects GABA A receptors.

Toxicity

The intraperitoneal LD50 in male mice is 1.87 g/kg. In reported cases of acute overdosage with acamprosate (doses of up to 56 grams of acamprosate calcium) diarrhea was the only reported symptom attributable to acamprosate. In the case of an overdose, supportive and symptomatic treatment is recommended.

Food Interaction

  • Take with or without food. Food decreases drug absorption, but not to a clinically significant extent.

[Minor] Administration with food may decrease the bioavailability of acamprosate.

The clinical significance is unknown.

Besobrial Disease Interaction

Major: renal impairmentModerate: depression

Volume of Distribution

At steady state concentrations, the distribution of acamprosate is about 20L. Following intravenous administration, the volume of distribution is about 72-109 L (an estimated 1 L/kg).

Elimination Route

Besobrial is absorbed in the gastrointestinal tract. The absolute bioavailability of acamprosate after oral administration is about 11%. The effect of food absorption is clinically insignificant and no adjustment of the dose is necessary with regard to meals. After repeated oral doses of 666 mg 3 times a day, steady-state concentrations are achieved within 5 to 7 days, with plasma concentration ranging between 370 to 650 micrograms/L.

Half Life

In pharmacokinetic studies, enteric-coated acamprosate tablets demonstrate a terminal elimination half-life 10-fold higher than reported 3 hour half-life after intravenous infusion of acamprosate. After two oral doses of acamprosate 333mg, the terminal half-life ranges between 20 - 33 hours.

Clearance

Severe renal insufficiency decreases the elimination of acamprosate, and is a contraindication. An acamprosate dose of 333mg, three times daily, is recommended for moderate renal impairment (creatinine clearance of 30-50 mL/min).

Elimination Route

Half of acamprosate excretion occurs as unchanged acetyl-homotaurine in urine, and the other half possibly by biliary excretion. The kidneys are primarily responsible for the elimination of acamprosate.

Innovators Monograph

You find simplified version here Besobrial

http://classyfire.wishartlab.com/tax_nodes/C0000000
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http://classyfire.wishartlab.com/tax_nodes/C0004557
http://classyfire.wishartlab.com/tax_nodes/C0000323
http://classyfire.wishartlab.com/tax_nodes/C0000278
http://classyfire.wishartlab.com/tax_nodes/C0003940
http://classyfire.wishartlab.com/tax_nodes/C0004150
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http://www.hmdb.ca/metabolites/HMDB0014797
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https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506657
https://www.chemspider.com/Chemical-Structure.64300.html
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=82819
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=51041
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL1201293
https://zinc.docking.org/substances/ZINC000001554588
http://bidd.nus.edu.sg/group/cjttd/ZFTTDDRUG.asp?ID=DAP000857
http://www.pharmgkb.org/drug/PA10344
http://www.rxlist.com/cgi/generic3/campral.htm
https://www.drugs.com/cdi/acamprosate.html
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/cam1691.shtml
https://en.wikipedia.org/wiki/Acamprosate
*** Taking medicines without doctor's advice can cause long-term problems.
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